Retinal dynamics underlie its switch from inverse agonist to agonist during rhodopsin activation
Andrey V Struts1, Gilmar F J Salgado, Karina Martínez-Mayorga
1Department of Chemistry, University of Arizona, Tucson, AZ, USA.
Abstract:
X-ray and magnetic resonance approaches, though central to studies of G protein-coupled receptor (GPCR)-mediated signaling, cannot address GPCR protein dynamics or plasticity. Here we show that solid-state (2)H NMR relaxation elucidates picosecond-to-nanosecond-timescale motions of the retinal ligand that influence larger-scale functional dynamics of rhodopsin in membranes. We propose a multiscale activation mechanism whereby retinal initiates collective helix fluctuations in the meta I-meta II equilibrium on the microsecond-to-millisecond timescale.
Related Concept Videos
Channel Rhodopsins
Rhodopsins belong to the family of cell surface proteins called G-protein coupled receptors,...
Photoreceptors and Visual Pathways
The Retina
Activation and Inactivation of G Proteins
The Two-State Receptor Model
The binding affinity of a drug determines its interaction with one...
Anatomy of the Eyeball


